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Letters in Organic Chemistry


ISSN (Print): 1570-1786
ISSN (Online): 1875-6255

Synthesis of Melphalan-Gem-Bisphosphonate Conjugation to Bone Tumors and Study of Affinity to Hydroxyapatite In Vitro

Author(s): Qinglin Jiang, Li Yang, Li Hai and Yong Wu

Volume 5 , Issue 3 , 2008

Page: [229 - 233] Pages: 5

DOI: 10.2174/157017808783955862

Price: $65


To develop a methodology for bone-specific delivery of drugs, a bone-targeting gem-bisphosphonate was used as a carrier of drugs. We had synthesized five compounds, which were a new class of potential bone-targeting reagents for bone tumors consisting of melphalan linked to a gem-bisphosphonate moiety through an amide linkage. The conjugates showed a high affinity to hydroxyapatite in vitro.

Keywords: Bone-targeting, gem-bisphosphonates, melphalan, bone tumors

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